UNC1062 is a highly selective tyrosine kinase inhibitor that specifically targets MERTK. This compound effectively suppresses MERTK-mediated downstream signaling, induces apoptosis in cell cultures, reduces colony formation in soft agar, and inhibits invasion of melanoma cells. Notably, UNC1062 demonstrates potent inhibition of MERTK kinase activity, with an IC50 of 1.1 nM and a Morrison Ki of 0.33 nM. It also displays specificity within the TAM family, exhibiting IC50 values of 60 nM for TYRO3 and 85 nM for AXL [1].

UNC1062 在体外有效抑制 MERTK 激酶活性（MERTK IC50 = 1.1 nM，Morrison Ki = 0.33 nM），并在 TAM 家族内显示出特异性（TYRO3 IC50 = 60 nM，AXL IC50 = 85 nM）。使用增加浓度的 UNC1062 处理 HMCB 和 G361 细胞，导致 MERTK 磷酸化显著的剂量依赖性减少[1]。